These authors contributed equally to this work.
Direct Copper-Catalyzed α-Arylation of Benzyl Phenyl Ketones with Aryl Iodides: Route towards Tamoxifen†
Article first published online: 9 NOV 2012
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 51, Issue 51, pages 12815–12819, December 14, 2012
How to Cite
Danoun, G., Tlili, A., Monnier, F. and Taillefer, M. (2012), Direct Copper-Catalyzed α-Arylation of Benzyl Phenyl Ketones with Aryl Iodides: Route towards Tamoxifen . Angew. Chem. Int. Ed., 51: 12815–12819. doi: 10.1002/anie.201206024
The CNRS, ENSCM, and ANR (grant ANR-07-CP2D-08, H2OFERCAT) are thanked for financial support.
- Issue published online: 10 DEC 2012
- Article first published online: 9 NOV 2012
- Manuscript Revised: 12 SEP 2012
- Manuscript Received: 27 JUL 2012
- ANR. Grant Number: ANR-07-CP2D-08
- homogeneous catalysis;
- synthetic methods
No activation needed: The first efficient method for direct α-arylation of non-activated or non-protected family of enolizable ketones with simple aryl iodides employs a catalytic copper system. The method shows potential for the easy and step-economical synthesis of tamoxifen, the most commonly administrated drug for the management of breast cancer. R, R′, R′′ = electron-donating or electron-withdrawing groups.